Group Title: BMC Pharmacology
Title: Bioavailability of dodeca-2E, 4E, 8E, 10E/Z-tetraenoic acid isobutylamides after oral administration in rats and distribution in various tissues
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 Material Information
Title: Bioavailability of dodeca-2E, 4E, 8E, 10E/Z-tetraenoic acid isobutylamides after oral administration in rats and distribution in various tissues
Series Title: BMC Pharmacology
Physical Description: Archival
Creator: Wölkart,Karin
Frye,Reginald
Derendorf,Hartmut
Butterweck,Veronika
Bauer,Rudolf
Publication Date: 2009
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General Note: Start pageA35
General Note: M3: 10.1186/1471-2210-9-S2-A35
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Bibliographic ID: UF00099947
Volume ID: VID00001
Source Institution: University of Florida
Holding Location: University of Florida
Rights Management: Open Access: http://www.biomedcentral.com/info/about/openaccess/
Resource Identifier: issn - 1471-2210
http://www.biomedcentral.com/1471-2210/9/S2/A35

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Meeting abstract
Bioavailability of dodeca-2E, 4E, 8E, I OE/Z-tetraenoic acid
isobutylamides after oral administration in rats and distribution in
various tissues
Karin W1olkart', Reginald Frye2, Hartmut Derendorf3, Veronika Butterweck3
and Rudolf Bauer* I

Address: 'Institute of Pharmaceutical Sciences, Department of Pharmacognosy, Karl Franzens University Graz, 8010 Graz, Austria, 2Department
of Pharmacy Practice, College of Pharmacy, University of Florida, Gainesville, FL 32610, USA and 3Department of Pharmaceutics, College of
Pharmacy, University of Florida, Gainesville, FL 32610, USA
Email: Rudolf Bauer* rudolf.bauer@uni-graz.at
* Corresponding author



from 15th Scientific Symposium of the Austrian Pharmacological Society (APHAR) Joint meeting with the Hungarian Society of Experimental and Clinical
Pharmacology (MFT) and the Slovenian Pharmacological Society (SDF)
Graz, Austria. 19-21 November 2009

Published: 12 November 2009
BMC Pharmacology 2009, 9(Suppl 2):A35 doi:10.1186/1471-2210-9-S2-A35


This abstract is available from: http://www.biomedcentral.com/1471-2210/9/S2/A35
2009 Wolkart et al; licensee BioMed Central Ltd.


Background
Preparations from Echinacea are among the best-selling
phytopharmaceuticals worldwide and have been widely
used for the treatment of common cold and various upper
respiratory infections. The most relevant active principles
of Echinacea extracts are alkamides, caffeic acid derivatives
(CADs) and glycoproteins/polysaccharides [1]. The main
alkamides in Echinacea preparations are the isomeric
dodeca-2E,4E,8E,10E/Z-tetraenoic acid isobutylamides
("tetraenes"). Until now, a limited number of pharmacok-
inetic studies with alkamides have been reported, but no
data exist about their distribution in tissues and transport
through the blood-brain barrier (BBB). Therefore, we eval-
uated the pharmacokinetics of dodeca-2E,4E,8E,10E/Z-
tetraenoic acid isobutylamides after a single oral dose
administration of 2.5 mg/kg in plasma as well as in liver
and four different brain regions (hippocampus, cerebral
cortex, striatum and cerebellum).

Methods
Plasma and tissues were collected after 8, 15, 30 minutes
and 1, 2, 3, and 6 hours after oral dosing and the concen-
trations were determined by a liquid chromatography tan-
dem mass spectrometry (LC-MS/MS) method with
benzanilide as internal standard using the respective [M-


HI+ ions, m/z 248/152 for the dodeca-2E,4E,8E,1OE/Z-
tetraenoic acid isobutylamides and m/z 198/105 for the
internal standard.

Results
The liphophilic constituents were rapidly absorbed and
well distributed to the examined tissues. The highest con-
centration was found in the striatum. The total tetraene
amount in plasma was calculated as AUCo-. (794
min ng/mL), which was about 13-45% of that found in
different brain parts (1764-6192 min- ng/mL), and 63%
of that in liver tissues (1254 min ng/g). The Cm. in
plasma was 26.4 ng/mL, while the Cm.x in the different
brain regions varied between 33.8 ng/g and 46.0 ng/g.

Conclusion
The results demonstrate that the dodeca-2E,4E,8E,10E/Z-
tetraenoic acid isobutylamides are bioavailable in rats
with a rapid passage across the blood-brain barrier.

Acknowledgements
Supported by the Erwin-Schrodinger scholarship (FWF) J2754-B05.

References
I. Bauer R: Chemistry, analysis and immunological investiga-
tions of Echinacea phytopharmaceuticals. In Immunomodulatory

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http://www.biomedcentral.com/1471-2210/9/S2/A35


Agents from Plants Edited by: Wagner H. Basel, Boston, Berlin: Birkhduser;
1999:41-88.
2. Woelkart K, Frye RF, Derendorf H, Bauer R, Butterweck V: Phar-
macokinetics and tissue distribution of dodeca-2E,
4E,8E, I OE/Z-tetraenoic acid isobutylamides after oral admin-
istration in rats. Plant Med 2009 in press.


Page 2 of 2
(page number not for citation purposes)


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